Journal
LETTERS IN APPLIED MICROBIOLOGY
Volume 40, Issue 3, Pages 212-217Publisher
WILEY
DOI: 10.1111/j.1472-765X.2005.01657.x
Keywords
cytotoxicity; minimum bacteriocidal concentration; minimum inhibitory concentration; Mycobacterium smegmatis
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Funding
- NATIONAL CENTER FOR RESEARCH RESOURCES [G12RR008124] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES [K22AI001812] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [S06GM008012, R25GM060424, R25GM069621, R25GM049011] Funding Source: NIH RePORTER
- NCRR NIH HHS [G12RR08124] Funding Source: Medline
- NIAID NIH HHS [K22 AI01812-02] Funding Source: Medline
- NIGMS NIH HHS [R25GM49011-05, R25 GM069621-01, S06 GM8012-33, R25GM60424-03] Funding Source: Medline
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Aims: Mycobacteria are a serious cause of infections in humans, with limited treatment options, as no new antibiotics have been developed against mycobacteria since the 1960s. In this study, the antimycobacterial activity of a small library of acetophenone (AP) compounds was analysed. Methods and Results: Twenty-three AP derivatives were examined for activity against mycobacteria using a microbroth assay. The compounds were bacteriostatic, with the most effective (cyclohexylacetophenone and piperidinoacetophenone) having minimal inhibitory concentrations of 246 mum. Active compounds tended to be more hydrophobic, and may work by alkylation of as yet undetermined intracellular target protein(s). Cytotoxicity against eukaryotic cells was also determined and appears to be unrelated to the bacteriostatic activity. Significance and Impact of the Study: AP may serve as a novel group of useful therapeutics against the mycobacteria.
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